tiospirone [Ligand Id: 101] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL35057 (Tiospirone, BMY-13859)
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
  • 8.67
1 CHEMBL35057_lig_chart_1 Dopamine D2 receptor Rat
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  • 5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
  • This target only has 1 pki data point
  • 0
2 CHEMBL35057_lig_chart_2 5-HT1A receptor HumanRat
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
  • This target only has 1 pki data point
  • 9.24
3 CHEMBL35057_lig_chart_3 Serotonin 2a (5-HT2a) receptor Rat
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  • 5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335]
  • This target only has 1 pki data point
  • 8.3
4 CHEMBL35057_lig_chart_4 5-HT2C receptor Human
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  • 5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406]
  • 5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
  • 7.1
5 CHEMBL35057_lig_chart_5 5-HT6 receptor HumanRat
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  • 5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305]
  • This target only has 1 pki data point
  • 9.2
6 CHEMBL35057_lig_chart_6 5-HT7 receptor Rat
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
ChEMBL Displacement of [3H]NPA from rat brain Dopamine receptor D2 B 8.67 pKi 2.14 nM Ki J. Med. Chem. (1996) 39: 143-148 [PMID:8568801]
ChEMBL Displacement of [3H]NPA from rat brain Dopamine receptor D2 B 8.68 pKi 2.1 nM Ki J. Med. Chem. (1996) 39: 143-148 [PMID:8568801]
ChEMBL Compound was measured for affinity at dopamine receptor D2 labeled with [3H]spiroperidol radioligand in striatum tissue B 7.66 pIC50 22 nM IC50 J. Med. Chem. (1991) 34: 1068-1072 [PMID:1672156]
ChEMBL Binding affinity against Dopamine receptor D2 receptor of rat corpus striatal tissue with [3H]spiperone B 8.08 pIC50 8.4 nM IC50 J. Med. Chem. (1991) 34: 3316-3328 [PMID:1683407]
5-HT1A receptor in Human [GtoPdb: 1] [UniProtKB: P08908]
GtoPdb - - 8.3 pKi - - - Eur J Pharmacol (1998) 355: 245-56 [PMID:9760039]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Affinity for 5-hydroxytryptamine 1A receptor labeled with [3H]8-OH-DPAT radioligand in hippocampus tissue B 7.74 pIC50 18 nM IC50 J. Med. Chem. (1991) 34: 1068-1072 [PMID:1672156]
ChEMBL Binding affinity against 5-hydroxytryptamine 1A receptor of rat hippocampal tissue with [3H]8-OH-DPAT B 8.55 pIC50 2.85 nM IC50 J. Med. Chem. (1991) 34: 3316-3328 [PMID:1683407]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL Displacement of [3H]-ketanserin from rat brain 5-hydroxytryptamine 2A receptor B 9.24 pKi 0.58 nM Ki J. Med. Chem. (1996) 39: 143-148 [PMID:8568801]
ChEMBL Binding affinity against rat 5-hydroxytryptamine 2 receptor in rat cerebral cortex tissue using [3H]spiperone as radioligand B 9.4 pIC50 0.4 nM IC50 J. Med. Chem. (1991) 34: 3316-3328 [PMID:1683407]
5-HT2C receptor in Human [GtoPdb: 8] [UniProtKB: P28335]
GtoPdb - - 8.3 pKi - - - J Pharmacol Exp Ther (2000) 295: 226-32 [PMID:10991983]
5-HT6 receptor in Human [GtoPdb: 11] [UniProtKB: P50406]
GtoPdb - - 6 pKi - - - J Neurochem (1996) 66: 47-56 [PMID:8522988]
5-HT6 receptor in Rat [GtoPdb: 11] [UniProtKB: P31388]
GtoPdb - - 7.1 pKi - - - J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]
5-HT7 receptor in Rat [GtoPdb: 12] [UniProtKB: P32305]
GtoPdb - - 9.2 pKi - - - J Pharmacol Exp Ther (1994) 268: 1403-10 [PMID:7908055]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]